CN1817346A - Benzoyl metronidazole dispersion tablets and preparation thereof - Google Patents
Benzoyl metronidazole dispersion tablets and preparation thereof Download PDFInfo
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- CN1817346A CN1817346A CN 200610066058 CN200610066058A CN1817346A CN 1817346 A CN1817346 A CN 1817346A CN 200610066058 CN200610066058 CN 200610066058 CN 200610066058 A CN200610066058 A CN 200610066058A CN 1817346 A CN1817346 A CN 1817346A
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Abstract
A dispersing tablet of benzoyl metronidazole is proportionally prepared from benzoyl metronidazole and medicinal additives including disintegrant and filler. Its advantages are high curative effect and quickly taking its effect. Its preparing process is also disclosed.
Description
Technical field
The present invention relates to the improvement pharmaceutical dosage form of benzoic methyl nitroazole, it compares rapid-action with common benzoic methyl nitroazole capsule, and the rapid release effect is obvious, and curative effect is conclusive.
Background technology
Benzoic methyl nitroazole (Benzoylmetronidazole) has another name called metronidazole benzoyl ester, is the nitroimidazoles medicine that anaerobe resistant of new generation, protozoacide infect.Oral back in gastrointestinal tract in several hours hydrolysis discharge metronidazole, pretend and use identically with metronidazole, be used for the treatment of anaerobe and parasitic infection.Now in tens country's listings such as English, method, moral, day, in November, 1993, this medicine was the infection essential drugs by The World Health Organization's approval to benzoic methyl nitroazole.Hebei Pharmaceutical Factory, Tianjin City at first succeeds in developing this product at home in nineteen ninety-five, and has developed the oral administration mixed suspension dosage form.At present, Shang Shi dosage form mainly contains capsule and oral administration mixed suspension at home, and is widely used clinically.
The oral back of benzoic methyl nitroazole is hydrolyzed into the metronidazole that plays a major role at intestinal, and the bactericidal mechanism of metronidazole is not illustrated as yet fully, and the nitroreductase of anaerobe plays an important role in the energy metabolism of sensitive strain.The nitroreduction of this product becomes a kind of cell toxicant, thereby acts on the DNA metabolic process of antibacterial, makes the fracture of its helical structure or blocks it and transcribe and duplicate and cause cell death.The mechanism of anti-ameba ruptures the protozoacide nitrogen chain for suppressing its redox reaction.As anaerobe resistant of new generation, protozoacide infection medicine, benzoic methyl nitroazole has oral absorption rapidly, fully, long half time, characteristics such as side effect is little.
Benzoic methyl nitroazole in the market mostly is common capsule and dry suspension, capsule and dried suspendible are the widely used oral dosage forms of field of medicaments, it has takes and stores and transports convenient and the stable advantage of medicine, but benzoic methyl nitroazole is often fully absorbed because of the medicine stripping slowly influences medicine.In addition, because each taking dose is bigger, often make troubles for the patient of old man, child and dysphagia.Require at present every day three times in the clinical treatment, each 2.The result of clinical practice shows that the rapid release problem of benzoic methyl nitroazole is unresolved all the time.
What have the rapid release function comprises dosage forms such as dispersible tablet, effervescent tablet.The characteristics of dispersible tablet (being advantage) are that tablet is met behind the water in the short as far as possible time (generally in 3 minutes) disintegrate and become very granule and form uniform suspension, therefore, compare with general tablet, dispersible tablet has good dispersing state, and disintegration time is short, the medicine stripping is rapid, absorb soon bioavailability height, characteristics such as taking convenience, can swallow, chew to contain and suck, especially be fit to old, young and the patient of difficulty that swallows.With effervescent tablet relatively, dispersible tablet does not need effervescent (as carbonate and solid organic acid) and water soluble adjuvant, does not need the gentle relative temperature in control room, and instructions of taking various (effervescent tablet can only water in dissolving back oral).In addition, the dispersible tablet production technology is identical with common non-coated tablet, and no specific (special) requirements does not need vacuum lyophilization and extra package, and production cost is low.Therefore advantage is conspicuous.
Summary of the invention
The present invention gropes through a large amount of tests, is developed into benzoyl metronidazole dispersion tablets, has solved the shortcoming that the conventional dosage forms onset is slow, bioavailability is low, has improved curative effect, has reduced side effect.
On the one hand, the invention provides a kind of pharmaceutical composition of benzoyl metronidazole dispersion tablets, contain benzoic methyl nitroazole and suitable pharmaceutic adjuvant in the said composition, the pharmaceutic adjuvant in the present composition includes but not limited to (benzoic methyl nitroazole is by 100 parts of calculating):
A. disintegrating agent:
Microcrystalline Cellulose: consumption is 2～30 parts;
Polyvinylpolypyrrolidone: consumption is 3～40 parts;
Carboxymethyl starch sodium: consumption is 3～15 parts;
Low-substituted hydroxypropyl cellulose: consumption is 2～16 parts;
Or cross-linking sodium carboxymethyl cellulose: consumption is 2～16 parts.
Preferred polyvinylpolypyrrolidone, 3～40 parts.
B. filler:
Amylum pregelatinisatum: consumption is 2～50 parts;
Dextrin: consumption is 2～30 parts;
Lactose: consumption is 2～30 parts;
Microcrystalline Cellulose: consumption is 2～30 parts;
Mannitol: consumption is 2～10 parts;
Preferably: shared 4～30 parts of lactose and microcrystalline Cellulose.
C. binding agent
Polyvinylpyrrolidone aqueous solution, concentration range are 1～15%, and consumption is 2～20 parts;
Starch slurry, consumption are 2～20 parts;
Or the hydroxypropyl emthylcellulose aqueous solution, consumption is 2～20 parts.
Preferred adhesive is 10% polyvinylpyrrolidone aqueous solution, 10 parts of consumptions.
D. lubricant:
Stearic acid: consumption is 0.2～2.5 part;
Polyethylene Glycol: consumption is 0.2～2.5 part (Polyethylene Glycol of multi-purpose solid);
Magnesium stearate: consumption is 0.2～2.5 part;
Or Pulvis Talci: consumption is 2～20 parts.
Preferred magnesium stearate, 0.2～2.5 part.
In the above-mentioned composition, most preferably comprise 100 parts of benzoic methyl nitroazoles, 15 parts of disintegrating agents, 10 parts of 30 parts of binding agents of filler, 0.2 part of lubricant.
The specific embodiment
Further set forth the present invention below in conjunction with specific embodiments, but not as limitation of the present invention.
Embodiment 1:1000 sheet consumption
Benzoic methyl nitroazole 320.0g
Lactose 55.0g
Microcrystalline Cellulose 45.0g
Crospolyvinylpyrrolidone 40.0g
10% polyvinylpyrrolidone K29/32 aqueous solution 10.0g
Magnesium stearate 4.6g
Preparation technology:
120 mesh sieves will be crossed after the benzoic methyl nitroazole micronized, again with polyvinylpolypyrrolidone, lactose, the microcrystalline Cellulose mix homogeneously of recipe quantity, with 10% polyvinylpyrrolidone aqueous solution is binding agent system soft material, 16 mesh sieves are granulated, 50 ℃ of-60 ℃ of dryings, 14 mesh sieve granulate add the magnesium stearate mixing, make tablet.
Embodiment 2:1000 sheet consumption
Benzoic methyl nitroazole 320.0g
Amylum pregelatinisatum 30.0g
Microcrystalline Cellulose 60.0g
Carboxymethyl starch sodium 45.0g
10% polyvinylpyrrolidone K29/32 aqueous solution 10.0g
Magnesium stearate 4.6g
Preparation technology:
120 mesh sieves will be crossed after the benzoic methyl nitroazole micronized, again with carboxymethyl starch sodium, amylum pregelatinisatum, the microcrystalline Cellulose mix homogeneously of recipe quantity, with 10% polyvinylpyrrolidone aqueous solution is binding agent system soft material, 16 mesh sieves are granulated, 50 ℃ of-60 ℃ of dryings, 14 mesh sieve granulate add the magnesium stearate mixing, make tablet.
More than described the preferred embodiment for the present invention, so it is not in order to limit the present invention.Those skilled in the art can not depart from the improvement of category of the present invention and spirit to embodiment disclosed herein.
Claims (7)
1, benzoyl metronidazole dispersion tablets, contain the benzoic methyl nitroazole and the pharmaceutic adjuvant for the treatment of effective dose, it is characterized in that described pharmaceutic adjuvant comprises disintegrating agent and filler, wherein disintegrating agent is selected from least a of microcrystalline Cellulose, polyvinylpolypyrrolidone, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, cross-linking sodium carboxymethyl cellulose; This filler is selected from least a in amylum pregelatinisatum, dextrin, lactose, microcrystalline Cellulose, the mannitol.
2, the described dispersible tablet of claim 1, wherein by 100 parts of benzoic methyl nitroazoles, described disintegrating agent consumption is 2～50 parts, the consumption of described filler is 5～100 parts.
3, the described dispersible tablet of claim 2, wherein pharmaceutic adjuvant also comprises at least a in binding agent, the lubricant, described binding agent is selected from least a in polyvinylpyrrolidone aqueous solution, starch slurry, the hydroxypropyl emthylcellulose aqueous solution, lubricant is selected from least a in stearic acid, magnesium stearate, Pulvis Talci, Polyethylene Glycol, the Stepanol MG, press 100 parts of calculating of benzoic methyl nitroazole, described adhesive consumption is 2～25 parts, described wetting agent consumption is 5～20 parts, and lubricant is 0.1～20 part.
4, the described dispersible tablet of claim 3, wherein disintegrating agent is a polyvinylpolypyrrolidone, and filler is a lactose, and binding agent is the polyvinylpyrrolidone aqueous solution; Lubricant is a magnesium stearate.
5, the described dispersible tablet of claim 4 is pressed 100 parts of calculating of benzoic methyl nitroazole, and wherein disintegrating agent comprises 3～40 parts of polyvinylpolypyrrolidone, and filler comprises totally 10～50 parts of lactose and microcrystalline Cellulose; Binding agent is that concentration range is 2～20 parts of the polyvinylpyrrolidone aqueous solutions of 1～15% (g/g); Lubricant is 0.1～2.5 part of a magnesium stearate.
6, the described dispersible tablet of claim 5 is pressed 100 parts of calculating of benzoic methyl nitroazole, and wherein the disintegrating agent polyvinylpolypyrrolidone is 15 parts, and filler comprises totally 30 parts of lactose and microcrystalline Cellulose; Binding agent is that concentration range is 10 parts of the polyvinylpyrrolidone aqueous solutions of 10% (g/g); Lubricant is 0.2 part of a magnesium stearate.
7, the preparation method of the described dispersible tablet of claim 1～6 is: will cross 120 mesh sieves after the benzoic methyl nitroazole micronized, again with the adjuvant mix homogeneously of recipe quantity, with 10% polyvinylpyrrolidone aqueous solution is binding agent system soft material, 16 mesh sieves are granulated, 50 ℃ of-60 ℃ of dryings, 14 mesh sieve granulate add the magnesium stearate mixing, make tablet.
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| Application Number | Priority Date | Filing Date | Title |
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| CN 200610066058 CN1817346A (en) | 2006-03-28 | 2006-03-28 | Benzoyl metronidazole dispersion tablets and preparation thereof |
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| CN 200610066058 CN1817346A (en) | 2006-03-28 | 2006-03-28 | Benzoyl metronidazole dispersion tablets and preparation thereof |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102349894A (en) * | 2011-08-18 | 2012-02-15 | 海南良方医药有限公司 | Benzoylmetronidazole composition and preparation method thereof |
| CN104586749A (en) * | 2014-12-25 | 2015-05-06 | 海南卫康制药(潜山)有限公司 | Metronidazole composition freeze-dried tablet and preparation method thereof |
| CN106137988A (en) * | 2016-01-14 | 2016-11-23 | 上海信谊万象药业股份有限公司 | A kind of metronidazole solid preparation and preparation method thereof |
| CN113975232A (en) * | 2021-10-22 | 2022-01-28 | 北京汇诚益健医药科技有限责任公司 | Pharmaceutical composition of metronidazole benzoate |
-
2006
- 2006-03-28 CN CN 200610066058 patent/CN1817346A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102349894A (en) * | 2011-08-18 | 2012-02-15 | 海南良方医药有限公司 | Benzoylmetronidazole composition and preparation method thereof |
| CN102349894B (en) * | 2011-08-18 | 2013-03-13 | 海南良方医药有限公司 | Benzoylmetronidazole composition and preparation method thereof |
| CN104586749A (en) * | 2014-12-25 | 2015-05-06 | 海南卫康制药(潜山)有限公司 | Metronidazole composition freeze-dried tablet and preparation method thereof |
| CN106137988A (en) * | 2016-01-14 | 2016-11-23 | 上海信谊万象药业股份有限公司 | A kind of metronidazole solid preparation and preparation method thereof |
| CN113975232A (en) * | 2021-10-22 | 2022-01-28 | 北京汇诚益健医药科技有限责任公司 | Pharmaceutical composition of metronidazole benzoate |
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